c-Met/STAT3-IN-2
c-Met/STAT3-IN-2 is a c-Met and STAT3 inhibitor with IC50 values of 0.20 μM and 0.74 μM, respectively. c-Met/STAT3-IN-2 inhibits c-Met and STAT3 phosphorylation, binds to the STAT3 SH2 domain, and blocks pTyr705 recognition. c-Met/STAT3-IN-2 induces cancer cell apoptosis (apoptosis) and G2/M phase arrest, upregulates P53, Bax, PUMA, caspases-3, -8, and -9, and downregulates Bcl-2. c-Met/STAT3-IN-2 has broad-spectrum anticancer activity, inhibits cancer cell proliferation, and exhibits lethal activity against various cancer cell lines. c-Met/STAT3-IN-2 shows minimal off-target inhibition of STK3, STK4, PI3Kdelta, and VEGFR3. c-Met/STAT3-IN-2 can be used for research related to colorectal cancer, leukemia, non-small cell lung cancer, and breast cancer cells.
For research use only. We do not sell to patients.
- CAS No.: 459193-26-1
- Formula: C23H21FN4S
- Molecular Weight:404.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
c-Met 0.20 μM (IC50) |
STAT3 0.74 μM (IC50) |
Caspase-3 |
Caspase-8 |
Caspase-9 |
Bax |
Bcl-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
3.04 μM
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Cytotoxicity against human HCT-116 colon cancer cells assessed by MTT assay.
Cytotoxicity against human HCT-116 colon cancer cells assessed by MTT assay.
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42767173 |
| WI-38 | IC50 |
74.07 μM
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Cytotoxicity against normal human WI-38 fibroblasts assessed by MTT assay.
Cytotoxicity against normal human WI-38 fibroblasts assessed by MTT assay.
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42767173 |
In Vitro
c-Met/STAT3-IN-2 (compound 17e) inhibits c-Met and STAT3 phosphorylation with IC50 values of 0.20 μM and 0.74 μM, respectively, and shows minimal inhibition of off-target kinases[1].
c-Met/STAT3-IN-2 (10 μM) exhibits broad-spectrum anticancer activity in the NCI-60 cell line panel, with a mean GI% of 58.5%[1].
c-Met/STAT3-IN-2 exhibits selective cytotoxicity against HCT-116 colon cancer cells with an IC50 of 3.04 μM and a selectivity index of 24.37 relative to WI-38 normal fibroblasts[1].
c-Met/STAT3-IN-2 induces a total apoptosis rate of 6.22% in HCT-116 cells[1].
c-Met/STAT3-IN-2 upregulates the pro-apoptotic proteins P53, Bax, PUMA, and caspases-3/8/9 in HCT-116 cells, and downregulates Bcl-2, increasing the Bax/Bcl-2 ratio by 6-fold[1].
c-Met/STAT3-IN-2 (3.04 μM; 24 h) induces G2/M cell cycle arrest in HCT-116 cells, increasing the G2/M phase cell population to 69.68%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 colon cancer cells
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Concentration:3.04 μM (IC50)
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Incubation Time:24 h
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Result:G2/M phase increased from 7.58% (0.1% DMSO) to 69.68% with 17e.
Doxorubicin resulted in 49.88%.
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Protocol for Cell Cycle
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Ki-67 Immunostaining Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 459193-26-1
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Molecular Weight 404.50
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Formula C23H21FN4S
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SMILES
FC1=CC=C(C2=CSC3=NC=NC(N4CCN(CC5=CC=CC=C5)CC4)=C32)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
c-Met/STAT3-IN-2 Related Classifications
HY-189693 Related Classifications
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